Literature Review
Acetaminophen, also known as N-acetyl-para-aminophenol (APAP) or paracetamol in many countries, is a non-
opioid analgesic and antipyretic agent utilized for treating pain and fever (Gerriets & Nappe, 2024). Formula:
C8H9NO2 .Molar Mass: 151.165 g·mol−1
Pharmacokinetics
Absorption: 63-89%. Intravenous (IV) administration of acetaminophen resulted in immediate and higher peak
plasma concentrations. The rectal route is preferred for administration to bypass first-pass metabolism, especially in
unconscious patients and children Protein Binding: negligible to 10–25% in overdos. Bioavailability: is
dose-dependent: it increases from 63% for 500 mg dose to 89% for 1000 mg dose Metabolism:
Paracetamol is metabolized primarily in the liver, mainly by glucuronidation and sulfation, and
the products are then eliminated in the urine .Only 2–5% of the drug is excreted unchanged in the
urine. Excretion: Kidney Elimination half Life: 1.9-2.5hrs (Forrest, Clements, & Prescott, 2012) Melting
Point: 169 °C (336 °F) (Karthikeyan, Glen, & Bender, 2005) Pregnancy Category:A (Wikipedia
Contributors, 2024). Maximum daily dose is based on all routes of administration and all products
containing acetaminophen ([Link], 2019).
Dosage Forms: Paracetamol is available in oral, suppository, and intravenous forms (Wikipedia
Contributors, 2024).Our selected dosage form is Orodispersable films
INDICATION OF ACETAMINOPHEN:
It is used for Acute pain Headaches, menstrual pain, musculoskeletal pain sprains/injury. Paracetamol is generally
accepted to have excellent GI tolerability and is consequently an analgesic of choice for patients at risk for adverse
GI Unlike aspirin and some other NSAIDs that reportedly increase the risk of GI bleeding at any dose. Paracetamol
often recommended as first line pain reliver for people with hypertension Pain is considerably more common among
old people. paracetamol may be the first choice for treating mild to moderate acute pain for old people (Alchin,
Dhar, Siddiqui, & Christo, 2022).
1
Aim: The aim of this study is to formulate oral disintegrating films .Our work has planned to in
cooperate API paracetamol to give analgesic effect .This dosage form is preferred because it has huge
potential in gaining patient compliance ,they are portable and donot need water to be swallowed.
Materials: Paracetamol (PCM) as active ingredient (125mg), Hydroxy propyl methyl cellulose (HPMC)
225mg as a water soluble polymer, Sodium lauryl sulphate (SLS) 25mg, Mannitol (50mg) used as
sweetening agent and Glycerol(0.4ml) as humectant.
Methadology
PreFormulation Studies: 1. Excipient compatibility , solubility of API, Identify potential excipients,
Dissolution in media, Melting point , Thermal analysis,Bulk Density (Maddela, Vemuri, Harshini, Chukka,
& Reddy Bhavanam, 1 C.E.).
preparation of casting solution (containing drug, polymer, plasticizer, sweetener and flavor), deaeration
of the solution, transfer of appropriate volume of solution into a mould, drying the casting solution,
cutting the final dosage form into strips (size 2x3 cm) to contain the desired amount of drug (125 mg),
packaging and storage. Different formulations were developed by varying polymer (hydroxypropyl
methyl cellulose) and plasticizer (glycerol) concentrations. Sweetening and flavoring agents were added
to make the formulation palatable (K. Upret, Kumar, Anand, & Chawla, 2014)
References
1. Gerriets, V., & Nappe, T. M. (2024). Acetaminophen. Retrieved from National Library of
Medicine website: [Link]
2. Li, Y., Hong, X., Liang, L., Wang, X., & Ladd‐Acosta, C. (2023). Association between
acetaminophen metabolites and CYP2E1 DNA methylation level in neonate cord blood
in the Boston Birth Cohort. Clinical Epigenetics, 15(1). [Link]
023-01551-4
3. Forrest, J. A., Clements, J. A., & Prescott, L. F. (2012). Clinical pharmacokinetics of
paracetamol. Clinical Pharmacokinetics, 7(2), 93–107.
[Link]
4. Karthikeyan, M., Glen, R. C., & Bender, A. (2005). General Melting Point Prediction
Based on a Diverse Compound Data Set and Artificial Neural Networks. Journal of
Chemical Information and Modeling, 45(3), 581–590. [Link]
5. Wikipedia Contributors. (2024, October 16). Paracetamol. Retrieved October 16, 2024,
from Wikipedia website: [Link]
Drugs.com_pregnancy-2
6. [Link]. (2019). Acetaminophen Dosage. Retrieved from [Link] website:
[Link]
7. Alchin, J., Dhar, A., Siddiqui, K., & Christo, P. J. (2022). Why paracetamol
(acetaminophen) is a suitable first choice for treating mild to moderate acute pain in
adults with liver, kidney or cardiovascular disease, gastrointestinal disorders, asthma, or
2
who are older. Current Medical Research and Opinion, 38(5), 1–15.
[Link]
8. Wikipedia Contributors. (2024, October 16). Paracetamol. Retrieved October 16, 2024,
from Wikipedia website: [Link]
Drugs.com_pregnancy-2
9. Maddela, S., Vemuri, S., Harshini, Chukka, N., & Reddy Bhavanam, P. (1 C.E.). Journal
of Cardiovascular Disease Research Formulation and In-vitro Evaluation of
Paracetamol and Ibuprofen Immediate Release Tablets by Solid Dispersion Technique.
Retrieved from
[Link]
10. K. Upret, Kumar, L., Anand, S. P., & Chawla, V. (2014). Formulation and evaluation of mouth
dissolving films of paracetamol. International Journal of Pharmacy and Pharmaceutical Sciences,
6(5), 200–202. Retrieved from
[Link]
_dissolving_films_of_paracetamol
